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Journal articles on the topic 'Apilimod'

Author: Grafiati

Published: 2 June 2025

Last updated: 31 July 2025

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1

Baranov, Maksim V., Frans Bianchi, and Geert van den Bogaart. "The PIKfyve Inhibitor Apilimod: A Double-Edged Sword against COVID-19." Cells 10, no. 1 (2020): 30. http://dx.doi.org/10.3390/cells10010030.

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The PIKfyve inhibitor apilimod is currently undergoing clinical trials for treatment of COVID-19. However, although apilimod might prevent viral invasion by inhibiting host cell proteases, the same proteases are critical for antigen presentation leading to T cell activation and there is good evidence from both in vitro studies and the clinic that apilimod blocks antiviral immune responses. We therefore warn that the immunosuppression observed in many COVID-19 patients might be aggravated by apilimod.

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2

Gayle, Sophia, Sean Landrette, Neil Beeharry, et al. "Identification of apilimod as a first-in-class PIKfyve kinase inhibitor for treatment of B-cell non-Hodgkin lymphoma." Blood 129, no. 13 (2017): 1768–78. http://dx.doi.org/10.1182/blood-2016-09-736892.

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Key Points Apilimod has broad anticancer activity in vitro and in vivo across all subtypes of B-NHL. Apilimod induces B-NHL cytotoxicity through a unique mechanism of action that involves the disruption of lysosomal function.

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Kang, Yuan-Lin, Yi-ying Chou, Paul W. Rothlauf, et al. "Inhibition of PIKfyve kinase prevents infection by Zaire ebolavirus and SARS-CoV-2." Proceedings of the National Academy of Sciences 117, no. 34 (2020): 20803–13. http://dx.doi.org/10.1073/pnas.2007837117.

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Virus entry is a multistep process. It initiates when the virus attaches to the host cell and ends when the viral contents reach the cytosol. Genetically unrelated viruses can subvert analogous subcellular mechanisms and use similar trafficking pathways for successful entry. Antiviral strategies targeting early steps of infection are therefore appealing, particularly when the probability for successful interference through a common step is highest. We describe here potent inhibitory effects on content release and infection by chimeric vesicular stomatitis virus (VSV) containing the envelope pr

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4

Cinato, Mathieu, Laurie Guitou, Amira Saidi та ін. "Apilimod alters TGFβ signaling pathway and prevents cardiac fibrotic remodeling". Theranostics 11, № 13 (2021): 6491–506. http://dx.doi.org/10.7150/thno.55821.

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Nelson, Elizabeth A., Julie Dyall, Thomas Hoenen, et al. "The phosphatidylinositol-3-phosphate 5-kinase inhibitor apilimod blocks filoviral entry and infection." PLOS Neglected Tropical Diseases 11, no. 4 (2017): e0005540. http://dx.doi.org/10.1371/journal.pntd.0005540.

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Ring, Julian, Sarah Schlienkamp, Jil Haase, et al. "LBP-034 Evaluation of the PIKfyve kinase inhibitor Apilimod against hepatitis E virus infections." Journal of Hepatology 80 (June 2024): S94. http://dx.doi.org/10.1016/s0168-8278(24)00601-9.

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Wisniewski, Jasmine P., Caleb Cheng, Bailey Jackson, et al. "Abstract 3300: Dual inhibition of PIKfyve and KRAS/MAPK as a potential for therapeutic strategy for pancreatic ductal adenocarcinoma." Cancer Research 84, no. 6_Supplement (2024): 3300. http://dx.doi.org/10.1158/1538-7445.am2024-3300.

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Abstract Background: PIKfyve is a lipid kinase that serves as the single source for PI(3,5)P2, a critical molecule for lysosome functions, including autophagy. Pancreatic Ductal Adenocarcinoma (PDAC) is known to utilize autophagy as well as other lysosome functions to survive in its harsh microenvironment. Considering the role of PIKfyve in autophagy, we hypothesized that PIKfyve is important for PDAC pathophysiology. Indeed, we screened multiple cell lines of different cancer lineages and found that PDAC cell lines were highly sensitive to PIKfyve inhibitors apilimod and ESK981. Given these r

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Grenier, Shea, Cheska Galapate, Yijuan Zhang, et al. "Abstract A096: PIKfyve as a potential therapeutic target in pancreatic cancer." Cancer Research 84, no. 2_Supplement (2024): A096. http://dx.doi.org/10.1158/1538-7445.panca2023-a096.

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Abstract A lack of effective treatments beyond surgical resection and chemotherapy contributes to the 12% five-year survival rate of pancreatic ductal adenocarcinoma (PDAC), underscoring the need to identify novel therapeutic approaches. Pharmacological inhibition of phosphatidylinositol 3-phosphate 5-kinase (PIKfyve) with small molecules has been demonstrated to have therapeutic effects in tauopathies, viral infection, and cancer; however, these compounds have not been evaluated in PDAC. The PIKfyve lipid kinase generates PI5P and/or PI(3,5)P2 from phosphoinositol (PI) or PI3P, respectively,

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Wada, Yumiko, Irma Cardinale, Artemis Khatcherian, et al. "Apilimod Inhibits the Production of IL-12 and IL-23 and Reduces Dendritic Cell Infiltration in Psoriasis." PLoS ONE 7, no. 4 (2012): e35069. http://dx.doi.org/10.1371/journal.pone.0035069.

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DeLiberty, Jonathan M., Clint A. Stalnecker, Kristina Drizyte-Miller, et al. "Abstract 4851: Improving the efficacy of dual ERK-MAPK and autophagy inhibition as a therapeutic strategy for pancreatic ductal adenocarcinoma." Cancer Research 83, no. 7_Supplement (2023): 4851. http://dx.doi.org/10.1158/1538-7445.am2023-4851.

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Abstract Pancreatic ductal adenocarcinoma (PDAC) is characterized by KRAS- and autophagy-dependent growth. We and others recently demonstrated that inhibition of the RAF-MEK-ERK pathway resulted in upregulated autophagy, and that dual treatment with the autophagy inhibitor hydroxychloroquine (HCQ)/chloroquine (CQ) and MEK or ERK inhibitors (MEKi, ERKi) synergistically blocked PDAC growth. These findings provided rationale for our initiation of Phase I/II clinical trials evaluating the combination of MEKi (binimetinib; NCT04132505) or ERKi (LY3214996; NCT04386057) with HCQ in PDAC. However, HCQ

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Sands, Bruce E., Eric W. Jacobson, Thomas Sylwestrowicz та ін. "Randomized, double-blind, placebo-controlled trial of the oral interleukin-12/23 inhibitor apilimod mesylate for treatment of active Crohnʼs disease". Inflammatory Bowel Diseases 16, № 7 (2010): 1209–18. http://dx.doi.org/10.1002/ibd.21159.

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Rihn, Suzannah J., Andres Merits, Siddharth Bakshi, et al. "A plasmid DNA-launched SARS-CoV-2 reverse genetics system and coronavirus toolkit for COVID-19 research." PLOS Biology 19, no. 2 (2021): e3001091. http://dx.doi.org/10.1371/journal.pbio.3001091.

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The recent emergence of Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2), the underlying cause of Coronavirus Disease 2019 (COVID-19), has led to a worldwide pandemic causing substantial morbidity, mortality, and economic devastation. In response, many laboratories have redirected attention to SARS-CoV-2, meaning there is an urgent need for tools that can be used in laboratories unaccustomed to working with coronaviruses. Here we report a range of tools for SARS-CoV-2 research. First, we describe a facile single plasmid SARS-CoV-2 reverse genetics system that is simple to genetical

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Adepoju, Adewusi John, Dayo Felix Latona, Oluwafemi Gbenga Olafare, Abel Kolawole Oyebamiji, Misbaudeen Abdul-Hammed, and Banjo Semire. "Molecular docking and pharmacokinetics studies of Curcuma longa (Curcumin) potency against Ebola virus." Ovidius University Annals of Chemistry 33, no. 1 (2022): 22–35. http://dx.doi.org/10.2478/auoc-2022-0004.

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Abstract The Ebola virus disease causing hemorrhagic fever in human, has been known for nearly about 40 years, with the most recent outbreak being in West Africa creating humanitarian crisis, where over 11,308 deaths were recorded as reported in 30th March, 2016 (World Health Organization). Till now, Ebola virus drugs have been far from achieving regulatory FDA approval, and coupled with toxicity of these drugs, it is become imperative to appraise the available trail drugs, as well as looking into alternative natural resources of tackling menace. Therefore, in silico methods were used to asses

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Johnson, Mathieu, and Sandra Turcotte. "Abstract 2599: Targeting SETD2-inactivated cells with STF-62247 leads to cell cycle arrest." Cancer Research 83, no. 7_Supplement (2023): 2599. http://dx.doi.org/10.1158/1538-7445.am2023-2599.

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Abstract The SETD2 gene encodes a histone methyltransferase responsible for the trimethylation of histone 3 on lysine 36 (H3K36me3). While this canonic function plays a role in the regulation of cellular processes such as transcription, alternative splicing, and DNA damage reparation, SETD2 is also important for the methylation of other proteins like EZH2, STAT1, and the cytoskeletal proteins actin and α-tubulin. Mutations in SETD2 are found in a broad range of cancers, including Clear Cell Renal Cell Carcinoma (ccRCC). Loss of chromosome 3p followed by the inactivation of the tumor suppressor

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Costa, Andréia Luiza Oliveira, Mike dos Santos, Giulia Caroline Dantas-Vieira, Rosálida Estevam Nazar Lopes, Rossiane Claudia Vommaro, and Érica S. Martins-Duarte. "Antiproliferative and Morphological Analysis Triggered by Drugs Contained in the Medicines for Malaria Venture COVID-Box Against Toxoplasma gondii Tachyzoites." Microorganisms 12, no. 12 (2024): 2602. https://doi.org/10.3390/microorganisms12122602.

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Toxoplasma gondii is a protozoan, and the etiologic agent of toxoplasmosis, a disease that causes high mortality in immunocompromised individuals and newborns. Despite the medical importance of toxoplasmosis, few drugs, which are associated with side effects and parasite resistance, are available for its treatment. Here, we show a screening of molecules present in COVID-Box to discover new hits with anti-T. gondii activity. COVID-Box contains 160 molecules with known or predicted activity against SARS-CoV-2. Our analysis selected 23 COVID-Box molecules that can inhibit the tachyzoite forms of

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Mamontov, Eugene, Yongqiang Cheng, Luke L. Daemen, et al. "Low rotational barriers for the most dynamically active methyl groups in the proposed antiviral drugs for treatment of SARS-CoV-2, apilimod and tetrandrine." Chemical Physics Letters 777 (August 2021): 138727. http://dx.doi.org/10.1016/j.cplett.2021.138727.

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Sbrissa, Diego, Ghassan Naisan, Ognian C. Ikonomov, and Assia Shisheva. "Apilimod, a candidate anticancer therapeutic, arrests not only PtdIns(3,5)P2 but also PtdIns5P synthesis by PIKfyve and induces bafilomycin A1-reversible aberrant endomembrane dilation." PLOS ONE 13, no. 9 (2018): e0204532. http://dx.doi.org/10.1371/journal.pone.0204532.

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Krausz, Sarah, Maria J. H. Boumans, Danielle M. Gerlag, et al. "Brief Report: A phase IIa, randomized, double-blind, placebo-controlled trial of apilimod mesylate, an interleukin-12/interleukin-23 inhibitor, in patients with rheumatoid arthritis." Arthritis & Rheumatism 64, no. 6 (2012): 1750–55. http://dx.doi.org/10.1002/art.34339.

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Oh, Ki-Kwang, Md Adnan, and Dong-Ha Cho. "New Insight into Drugs to Alleviate Atopic March via Network Pharmacology-Based Analysis." Current Issues in Molecular Biology 44, no. 5 (2022): 2257–74. http://dx.doi.org/10.3390/cimb44050153.

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In the present study, a subject of atopic dermatitis (AD) is exposed progressively to allergic rhinitis (AR) and asthma (AS), which is defined as atopic march (AM). However, both the targets and compounds against AM are still largely unknown. Hence, we investigated the overlapping targets related directly to the occurrence and development of AD, AR, and AS through public databases (DisGeNET, and OMIM). The final overlapping targets were considered as key targets of AM, which were visualized by a Venn diagram. The protein–protein interaction (PPI) network was constructed using R package softwar

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Bouhamdani, Nadia, and Sandra Turcotte. "Abstract 3956: Identifying PIKfyve as potential target in clear cell renal cell carcinoma with a loss of the von Hippel-Lindau tumor suppressor gene." Cancer Research 83, no. 7_Supplement (2023): 3956. http://dx.doi.org/10.1158/1538-7445.am2023-3956.

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Abstract Background. Clear cell renal cell carcinoma (ccRCC) is the most frequent type of cancer in the kidney. These tumors are highly vascular and correlate with poor prognosis. Biallelic inactivation of the von Hippel-Lindau (VHL) tumor suppressor gene is a truncal event of ccRCC carcinogenesis, which yields new insights for targeted therapy. Our studies identified a small molecule, STF-62247, that is toxic to cells lacking VHL compared to RCC with a functional gene. We reported that STF-62247 blocks late stages of autophagy by targeting lysosome dynamics. Moreover, we identified lysosomal

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Cai, Xinming, Yongyao Xu, Atwood K. Cheung, et al. "PIKfyve, a Class III PI Kinase, Is the Target of the Small Molecular IL-12/IL-23 Inhibitor Apilimod and a Player in Toll-like Receptor Signaling." Chemistry & Biology 20, no. 7 (2013): 912–21. http://dx.doi.org/10.1016/j.chembiol.2013.05.010.

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Stewart, A. Keith, Zhihua Li, Olga Issakova, Nikolai Sepetov, and Suzanne Trudel. "PIK-001 a Novel Small Molecule Inhibitor of Pikfyve for Treatment of Multiple Myeloma (MM)." Blood 138, Supplement 1 (2021): 1602. http://dx.doi.org/10.1182/blood-2021-151208.

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Abstract We utilized ex vivo chemo-genomics screening to identify potentially unrecognized targets of plasma cell biology. Medium throughput screening on MM and NHL cell lines was conducted using a panel of known FDA-approved oncology drugs, kinase inhibitors, and epigenetic compounds assembled by the investigators. A refined panel was then selected and sensitivity to the single agents was evaluated in 25 MM and 15 NHL cell lines. One panel drug APY-0201 and related drugs such as apilimod were initially developed as suppressors of production of interleukin (IL)-12 and IL-23 production and ente

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Cormier, Jolène, and Sandra Turcotte. "Abstract 3617: Investigating a role for PIKfyve in cell migration and invasion of clear cell renal cell carcinoma." Cancer Research 83, no. 7_Supplement (2023): 3617. http://dx.doi.org/10.1158/1538-7445.am2023-3617.

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Abstract Introduction. Clear cell renal cell carcinoma (ccRCC) is the most frequent type of kidney cancer. These highly vascularized tumors are characterized by mutations that inactivate the von Hippel-Lindau (VHL) tumor suppressor gene. About 30 % of patients present metastasis at diagnosis and 30-40% of patients with localized tumors relapse after surgery. Unfortunately, metastatic ccRCC remains incurable and are resistant to standard therapies. Our studies demonstrated that ccRCC with a loss of VHL can be targeted using a small molecule named STF-62247. This molecule blocks the autophagic f

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Baral, Garima, Claire M. Pfeffer, Indiraa Doraivel, Sara N. Filippelli та Brittany L. Allen-Petersen. "Abstract 4374: PP2A-B56α in nutrient scavenging: Tipping the balance from macropinocytosis to cell death in pancreatic cancer". Cancer Research 84, № 6_Supplement (2024): 4374. http://dx.doi.org/10.1158/1538-7445.am2024-4374.

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Abstract Pancreatic Ductal Adenocarcinoma (PDAC) is the fourth leading cause of cancer related deaths in the US, with the lowest five-year survival rate of all major cancers. Nutrients in the PDAC microenvironment are commonly depleted, with the vital amino acid glutamine among the most deficient metabolites. To circumvent this deprivation, PDAC cells initiate KRAS dependent macropinocytosis, an actin-driven nutrient scavenging pathway. Macropinosomes fuse with lysosomes in a process mediated by the kinase PIKfyve. It allows cells to replenish the nutrients required for survival. As glutamine

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Pakkan, Ruya, Caleb Cheng, Jasmine Wisniewski, et al. "Abstract 4158: PIKfyve inhibition drives lipogenic adaptation and reveals metabolic vulnerabilities in PDAC." Cancer Research 85, no. 8_Supplement_1 (2025): 4158. https://doi.org/10.1158/1538-7445.am2025-4158.

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Abstract PIKfyve plays a key role in autophagy and lysosomal functions, which are critical for pancreatic ductal adenocarcinoma (PDAC) cell metabolism and survival. Consistent with this, we found that PIKfyve perturbation suppresses autophagy and reduces PDAC cell viability. Prior studies show that autophagy and lysosomal processes are critical for maintaining iron homeostasis and mitochondrial respiration in PDAC. However, PIKfyve inhibition did not seem to significantly affect oxygen consumption rate (OCR) compared to other lysosomal inhibitors such as chloroquine and bafilomycin, suggesting

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DeLiberty, Jonathan M., Mallory K. Roach, Clint A. Stalnecker, et al. "Abstract C026: Concurrent inhibition of the RAS ERK-MAPK pathway and PIKfyve as a therapeutic strategy for pancreatic cancer." Cancer Research 84, no. 17_Supplement_2 (2024): C026. http://dx.doi.org/10.1158/1538-7445.pancreatic24-c026.

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Abstract Pancreatic ductal adenocarcinoma (PDAC) is characterized clinically by poor survival and mechanistically by KRAS- and autophagy-dependent growth. We and others previously demonstrated that inhibition of KRAS signaling via downstream inhibition of the RAF-MEK-ERK pathway enhanced autophagic flux and dependency of PDAC on autophagy. Furthermore, we demonstrated that concurrent treatment with the nonspecific autophagy inhibitor chloroquine (CQ) and ERK MAPK inhibitors synergistically blocked PDAC growth. These findings provided rationale for our initiation of Phase I/II clinical trials e

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Roach, Mallory K., Jonathan M. DeLiberty, Elyse G. Schechter, et al. "Abstract C036: Vertical inhibition of the autophagy pathway enhances sensitization to RAS MAPK pathway inhibition in pancreatic ductal adenocarcinoma." Cancer Research 84, no. 17_Supplement_2 (2024): C036. http://dx.doi.org/10.1158/1538-7445.pancreatic24-c036.

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Abstract PDAC growth is characterized by dependencies on both mutant KRAS signaling and autophagy. Our group and others previously demonstrated that inhibition of the RAF/MEK/ERK pathway in PDAC induces an increased dependence on autophagy, a metabolic nutrient scavenging process by which cellular components are recycled in times of nutrient stress. Combined inhibition of the ERK MAPK pathway and autophagy inhibited the growth of multiple preclinical models of PDAC. Based on these findings, combined ERK/MEK inhibition and hydroxychloroquine (HCQ) is currently under clinical evaluation (NCT0382

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DeLiberty, Jonathan M., Mallory K. Roach, Noah L. Pieper, et al. "Abstract C047: Improving the efficacy of dual ERK-MAPK and autophagy inhibition as a therapeutic strategy for pancreatic ductal adenocarcinoma." Cancer Research 84, no. 2_Supplement (2024): C047. http://dx.doi.org/10.1158/1538-7445.panca2023-c047.

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Abstract Pancreatic ductal adenocarcinoma (PDAC) is characterized by KRAS- and autophagy-dependent growth. We and others recently demonstrated that inhibition of KRAS signaling through targeting the RAF-MEK-ERK kinase cascade resulted in further reliance on autophagy. We found that targeting this increased reliance on autophagy with the autophagy inhibitor hydroxychloroquine (HCQ)/chloroquine (CQ) together with MEK or ERK inhibition (MEKi, ERKi) synergistically blocked PDAC growth. These findings provided rationale for our initiation of Phase I/II clinical trials evaluating the combination of

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Wisniewski, Jasmine P., Caleb Cheng, Sydney Peters, et al. "Abstract 6667: Dual inhibition of PIKfyve and KRAS/MAPK targets metabolic vulnerabilities of pancreatic ductal adenocarcinoma." Cancer Research 85, no. 8_Supplement_1 (2025): 6667. https://doi.org/10.1158/1538-7445.am2025-6667.

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Abstract Background: Pancreatic Ductal Adenocarcinoma (PDAC) exists within a harsh, nutrient-depleted microenvironment, and is known to use lysosomal processes, such as autophagy, for maintenance of metabolic function. PIKfyve is a lipid kinase that serves as the single source for PI(3, 5)P2, a molecule critical for the process of autophagy. Considering the role of PIKfyve in autophagy, we hypothesized it to be crucial for PDAC pathophysiology. Methods & Results: To evaluate the significance of PIKfyve in PDAC, we employed RNA-ISH and found that PIKfyve was significantly higher expressed i

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Magid Diefenbach, Catherine S., Jonathan B. Cohen, Wael A. Harb, et al. "Results of a completed phase I study of LAM-002 (apilimod dimesylate), a first-in-class phosphatidylinositol-3-phosphate 5 kinase (PIKfyve) inhibitor, administered as monotherapy or with rituximab or atezolizumab to patients with previously treated follicular lymphoma or other B-cell cancers." Journal of Clinical Oncology 38, no. 15_suppl (2020): 8017. http://dx.doi.org/10.1200/jco.2020.38.15_suppl.8017.

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8017 Background: LAM-002 is a selective inhibitor of PIKfyve that disrupts lysosomal homeostasis, inducing cytotoxicity in B-cell lymphoma models as monotherapy or with anti-CD20 or anti-PDL1 antibodies (Gayle et al., Blood 2017;129(13):1768). Methods: In this study, patients received LAM-002 orally 2-3 times per day (BID or TID) in a 3+3 escalation. Additional patients received LAM-002 125 mg BID as monotherapy; with rituximab 375 mg/m2 intravenously (IV) and or subcutaneously weekly (Q1W) x 4 → Q8W x 4; or atezolizumab 1200 mg IV Q3W until disease progression or unacceptable toxicity. Pharma

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DeLiberty, Jonathan M., Ryan Robb, Mallory K. Roach, et al. "Abstract IA-06: Elucidation of metabolic resistance mechanisms to RAS inhibition." Cancer Research 84, no. 17_Supplement_2 (2024): IA—06—IA—06. http://dx.doi.org/10.1158/1538-7445.pancreatic24-ia-06.

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Abstract Pancreatic ductal adenocarcinoma (PDAC) is characterized by KRAS- and autophagy-dependent growth. We previously determined that concurrent inhibition of autophagy, using the lysosomal inhibitor chloroquine (CQ), and of ERK, using a small molecule ERK inhibitor (ERKi), synergistically suppressed the growth of pancreatic ductal adenocarcinoma (PDAC) cell lines and patient xenograft-derived (PDX) organoids in vitro and PDX tumors in vivo. Our findings provided the rationale for our initiation of Phase I and Phase I/II clinical trials evaluating the combination of MEKi (binimetinib; NCT04

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Cheng, Caleb, Jasmine P. Wisniewski, Ahmet Korkaya, et al. "Abstract 2087: Targeting lipid metabolism in pancreatic cancer." Cancer Research 84, no. 6_Supplement (2024): 2087. http://dx.doi.org/10.1158/1538-7445.am2024-2087.

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Abstract Background PIKfyve is a lipid kinase that serves as the sole source of cellular PI(3,5)P2 and PI5P, critical phosphatidylinositols for autophagy and lysosome function. Pancreatic ductal adenocarcinoma (PDAC) is known to upregulate and depend on lysosomal functions such as autophagy to exist in its harsh, nutrient-disrupted microenvironment. Thus, we aimed to establish PIKfyve as a therapeutic target in PDAC. Using a PIKfyve-knockout genetically engineered mouse model of pancreatic cancer (KC and KPC), we determined that PIKfyve was necessary for PDAC development. Given these results,

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Coma, Silvia, Xiuting Liu, Noah L. Pieper, et al. "Abstract A091: The RAF/MEK clamp avutometinib as the backbone of therapy for pancreatic cancer: Novel combinations with standard of care chemotherapy, FAK inhibitors, KRAS G12D inhibitors and/or autophagy inhibitors." Cancer Research 84, no. 2_Supplement (2024): A091. http://dx.doi.org/10.1158/1538-7445.panca2023-a091.

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Abstract KRAS mutations (mt) occur in up to 98% of pancreatic ductal adenocarcinoma (PDAC) and represent a key initiating event in PDAC carcinogenesis. Therapeutic efforts targeting the RAS/RAF/MEK/ERK (MAPK) pathway with MEK-only inhibitors have been unsuccessful in substantially modifying PDAC prognosis. Thus, novel strategies are needed to overcome putative mechanisms of resistance to MEK inhibition such as focal adhesion kinase (FAK) pathway activation. Another hallmark of PDAC is its high stromal density, which is thought to limit the penetration of cytotoxic drugs and T cells into the tu

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STEPANYUK, L. M., O. B. VYSOTSKY, S. I. KURYLO, T. I. DOVBUSH, and N. O. KOVALENKO. "U-Pb isotopes geochronology by monazite of granitoids of Krynychuvatsky massive (Ingul megablock of the Ukrainian Shield)." Geology and Mineral Resources of World Ocean 20, no. 1 (2024): 77–82. http://dx.doi.org/10.15407/gpimo2024.01.077.

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Pegmatite (sample 13/10) exposed in the valley of the Berezivka River (Krynychuvatka village) was studied and its isotopic age was determined by monazite. Granitoids of the Krynichuvatsky massif differ from other granitoids of the Kirovohrad complex in their petrographic composition (mainly plagioclase, plagioclase-microcline), structural (aplitoid, pegmatoid inclusions) and texture (in some areas, aplitoid granites are characterized by linearly oriented grains of lamellar (lenticular) quartz, elongated feldspar crystals) and the composition of xenoliths (amphibolites, amphibole-biotite, bioti

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Morris, Patrick J., Curtis Moore, and Craig J. Thomas. "Apilimod." IUCrData 2, no. 5 (2017). http://dx.doi.org/10.1107/s2414314617006939.

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Apilimod {systematic name:N-[(E)-(3-methylbenzylidene)amino]-6-(morpholin-4-yl)-2-[2-(pyridin-2-yl)ethoxy]pyrimidin-4-amine}, C23H26N6O2, a molecule of interest for its antiviral properties, was acquired from several different commercial vendors. Analysis of several commercial batches had led to some ambiguity over the exact structure. In order to remove any ambiguity, the structure was confirmed by X-ray crystallography. In addition, the NMR spectra are provided as reference material for future investigations.

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Hou, Yingting, Hongbin He, Ming Ma, and Rongbin Zhou. "Apilimod activates the NLRP3 inflammasome through lysosome-mediated mitochondrial damage." Frontiers in Immunology 14 (June 8, 2023). http://dx.doi.org/10.3389/fimmu.2023.1128700.

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NLRP3 is an important innate immune sensor that responses to various signals and forms the inflammasome complex, leading to IL-1β secretion and pyroptosis. Lysosomal damage has been implicated in NLRP3 inflammasome activation in response to crystals or particulates, but the mechanism remains unclear. We developed the small molecule library screening and found that apilimod, a lysosomal disruptor, is a selective and potent NLRP3 agonist. Apilimod promotes the NLRP3 inflammasome activation, IL-1β secretion, and pyroptosis. Mechanismically, while the activation of NLRP3 by apilimod is independent

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Goettsch, C., N. Hense, B. Mir, and N. Marx. "The role of endomembrane homeostasis in vascular calcification." European Heart Journal 44, Supplement_2 (2023). http://dx.doi.org/10.1093/eurheartj/ehad655.3239.

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Abstract Background Cardiovascular diseases are a leading cause of mortality, with cardiovascular calcification as a prominent predictor and contributor. Microcalcifications in thin fibrous caps of atherosclerotic plaques create biomechanical instability, leading to plaque vulnerability. Recent work indicated that cellular-derived extracellular vesicles (EVs) are pivotal for microcalcification nucleation. EVs can originate from the endolysosomal system, and FYVE-Type Zinc Finger Containing Phosphoinositide Kinase (PIKfyve), a lipid kinase, plays a key role in the endolysosomal maturation. Purp

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Babu, Suma, Katharine A. Nicholson, Jeffrey D. Rothstein, et al. "Apilimod dimesylate in C9orf72 amyotrophic lateral sclerosis: a randomized phase 2a clinical trial." Brain, April 12, 2024. http://dx.doi.org/10.1093/brain/awae109.

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Abstract Apilimod dimesylate is a first-in-class phosphoinositide kinase, FYVE-type zinc finger containing (PIKfyve) inhibitor with favourable clinical safety profile and has demonstrated activity in preclinical C9orf72 and TDP-43 amyotrophic lateral sclerosis models. In this amyotrophic lateral sclerosis clinical trial, the safety, tolerability, CNS penetrance, and modulation of pharmacodynamic target engagement biomarkers were evaluated. This Phase 2a, randomized, double-blind, placebo-controlled, biomarker-endpoint clinical trial was conducted in four USA centres (ClinicalTrials.gov NCT0516

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Verma, Soumya, Amit Dubey, Rashika Singh, Rajratna Tayade, and Vipin Kumar Mishra. "In‐Silico Screening, Molecular Dynamics, and DFT Analysis of ZINC and ChEMBL Library Compounds for SARS‐CoV‐2 Main Protease Inhibition." ChemistrySelect 10, no. 4 (2025). https://doi.org/10.1002/slct.202403269.

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AbstractAlthough COVID‐19 is no longer classified as a global emergency, the emergence of SARS‐CoV‐2 variants highlights the urgent need for antiviral drug discovery. This study identifies potent inhibitors of the SARS‐CoV‐2 main protease, supporting future preparedness and advancing antiviral strategies. Using experimental drugs from the ZINC and ChEMBL libraries, a systematic workflow combining SwissSimilarity‐based screening, molecular docking, molecular dynamics (MD) simulations, and density functional theory (DFT) calculations was employed for robust candidate assessment. Five potential i

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Kreutzberger, Alex J. B., Anwesha Sanyal, Ravi Ojha, et al. "Synergistic block of SARS-CoV-2 infection by combined drug inhibition of the host entry factors PIKfyve kinase and TMPRSS2 protease." Journal of Virology, August 18, 2021. http://dx.doi.org/10.1128/jvi.00975-21.

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Repurposing FDA-approved inhibitors able to prevent infection by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) could provide a rapid path to establish new therapeutic options to mitigate the effects of coronavirus disease 2019 (COVID-19). Proteolytic cleavages of the spike S protein of SARS-CoV-2, mediated by the host cell proteases cathepsin and TMPRSS2, alone or in combination, are key early activation steps required for efficient infection. The PIKfyve kinase inhibitor apilimod interferes with late endosomal viral traffic, and through an ill-defined mechanism prevents in vitr

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Logue, James, Arup R. Chakraborty, Robert Johnson, et al. "PIKfyve-specific inhibitors restrict replication of multiple coronaviruses in vitro but not in a murine model of COVID-19." Communications Biology 5, no. 1 (2022). http://dx.doi.org/10.1038/s42003-022-03766-2.

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AbstractThe ongoing COVID-19 pandemic has claimed more than 6 million lives and continues to test the world economy and healthcare systems. To combat this pandemic, the biological research community has shifted efforts to the development of medical countermeasures, including vaccines and therapeutics. However, to date, the only small molecules approved for the treatment of COVID-19 in the United States are the nucleoside analogue Remdesivir and the protease inhibitor Paxlovid, though multiple compounds have received Emergency Use Authorization and many more are currently being tested in human

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Saffi, Golam. "Lysosome enlargement in PIKfyve inhibited cells proceeds through homotypic lysosome fusion rather than growth of individual lysosomes." FASEB Journal 31, S1 (2017). http://dx.doi.org/10.1096/fasebj.31.1_supplement.629.12.

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Phosphoinositides are important lipids that modulate various functions including signal transduction, membrane trafficking, and organelle identity. Phosphatidylinositol‐3,5‐bisphosphate [PI(3,5)P2] is a phosphoinositide found on lysosomes where it controls a wide array of functions such as stress‐induced signalling, autophagic flux, ion‐channel activity, trafficking and endolysosome morphology. Lysosomes are degradative organelles where macromolecules, foreign pathogens, and intracellular organelles arrive through endocytosis, phagocytosis and autophagy for degradation, respectively. PI(3,5)P2

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Chen, Xinlu, Luyao Gong, Yuanyuan Wang, et al. "IL-23 inhibitor enhances the effects of PTEN DNA-loaded lipid nanoparticles for metastatic CRPC therapy." Frontiers in Pharmacology 15 (June 5, 2024). http://dx.doi.org/10.3389/fphar.2024.1388613.

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Introduction: Metastatic castration-resistant prostate cancer (mCRPC) patients face challenges due to limited treatment options. About 50% of patients with mCRPC have a functional loss of phosphatase and tensin homology deleted on chromosome 10 (PTEN), leading to tumor progression, metastasis, and immune suppression. Moreover, elevated IL-23 produced by myeloid-derived suppressor cells (MDSCs) is found in CRPC patients, driving tumor progression. Therefore, a combination strategy based on PTEN restoration and IL-23 inhibition may block CRPC progression and metastasis.Methods: The antitumor eff

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Choi, Jae Eun, Yuanyuan Qiao, Ilona Kryczek, et al. "PIKfyve, expressed by CD11c-positive cells, controls tumor immunity." Nature Communications 15, no. 1 (2024). http://dx.doi.org/10.1038/s41467-024-48931-9.

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AbstractCancer treatment continues to shift from utilizing traditional therapies to targeted ones, such as protein kinase inhibitors and immunotherapy. Mobilizing dendritic cells (DC) and other myeloid cells with antigen presenting and cancer cell killing capacities is an attractive but not fully exploited approach. Here, we show that PIKFYVE is a shared gene target of clinically relevant protein kinase inhibitors and high expression of this gene in DCs is associated with poor patient response to immune checkpoint blockade (ICB) therapy. Genetic and pharmacological studies demonstrate that PIK

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Miner, Gregory E., and Rutilio A. Fratti. "Phosphatidylinositol 3,5‐Bisphosphate acts as a Novel Regulator of Calcium Transport During Saccharomyces Cerevisiae vacuolar fusion." FASEB Journal 31, S1 (2017). http://dx.doi.org/10.1096/fasebj.31.1_supplement.630.18.

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Phosphoinositides (PIs) are a group of lipids that are differentially phosphorylated to provide specific protein‐lipid interactions that are necessary in maintaining eukaryotic homeostasis. In membrane traffic, different PIs can interact with nucleotide exchange factors, tethering molecules and SNARE proteins ultimately leading to membrane fusion and transfer of cargo material. Our work has shown that phosphatidylinositol 3‐phosphate (PI3P), PI4P and PI(4,5)P2 are essential for the fusion of yeast vacuoles/lysosomes. However, little is known about the role of PI(3,5)P2 in the fusion pathway. O

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Wible, Daric J., Zalak Parikh, Eun Jeong Cho, et al. "Unexpected inhibition of the lipid kinase PIKfyve reveals an epistatic role for p38 MAPKs in endolysosomal fission and volume control." Cell Death & Disease 15, no. 1 (2024). http://dx.doi.org/10.1038/s41419-024-06423-0.

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Abstractp38 mitogen-activated protein kinases (MAPKs) participate in autophagic signaling; and previous reports suggest that pyridinyl imidazole p38 MAPK inhibitors, including SB203580 and SB202190, induce cell death in some cancer cell-types through unrestrained autophagy. Subsequent studies, however, have suggested that the associated cytoplasmic vacuolation resulted from off-target inhibition of an unidentified enzyme. Herein, we report that SB203580-induced vacuolation is rapid, reversible, and relies on the class III phosphatidylinositol 3-kinase (PIK3C3) complex and the production of pho

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Lu, Jiang‐Tao, Meng‐Ke Xiao, Ying‐Ying Feng, et al. "Apilimod enhances specific productivity in recombinant CHO cells through cell cycle arrest and mediation of autophagy." Biotechnology Journal, December 7, 2022, 2200147. http://dx.doi.org/10.1002/biot.202200147.

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Howell, Rowan, Matthew A. Clarke, Ann-Kathrin Reuschl, et al. "Executable network of SARS-CoV-2-host interaction predicts drug combination treatments." npj Digital Medicine 5, no. 1 (2022). http://dx.doi.org/10.1038/s41746-022-00561-5.

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AbstractThe COVID-19 pandemic has pushed healthcare systems globally to a breaking point. The urgent need for effective and affordable COVID-19 treatments calls for repurposing combinations of approved drugs. The challenge is to identify which combinations are likely to be most effective and at what stages of the disease. Here, we present the first disease-stage executable signalling network model of SARS-CoV-2-host interactions used to predict effective repurposed drug combinations for treating early- and late stage severe disease. Using our executable model, we performed in silico screening

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Chu, Yunpeng, Muyun Wei, Zhongyu Cao, et al. "Integrative analysis based on CRISPR screen identifies apilimod as a potential therapeutic agent for cisplatin-induced acute kidney injury treatment." Science China Life Sciences, March 21, 2025. https://doi.org/10.1007/s11427-025-2874-8.

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Shema Mugisha, Christian, Hung R. Vuong, Maritza Puray-Chavez, et al. "A Simplified Quantitative Real-Time PCR Assay for Monitoring SARS-CoV-2 Growth in Cell Culture." mSphere 5, no. 5 (2020). http://dx.doi.org/10.1128/msphere.00658-20.

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ABSTRACT Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has infected millions within just a few months, causing severe respiratory disease and mortality. Assays to monitor SARS-CoV-2 growth in vitro depend on time-consuming and costly RNA extraction steps, hampering progress in basic research and drug development efforts. Here, we developed a simplified quantitative real-time PCR assay that bypasses viral RNA extraction steps and can monitor SARS-CoV-2 growth from a small amount of cell culture supernatants. In addition, we show that this approach is easily adaptable to numerous

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